280773-85-5Relevant academic research and scientific papers
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor
Zhang, Penglie,Huang, Wenrong,Wang, Lingyan,Bao, Liang,Jia, Zhaozhong J.,Bauer, Shawn M.,Goldman, Erick A.,Probst, Gary D.,Song, Yonghong,Su, Ting,Fan, Jingmei,Wu, Yanhong,Li, Wenhao,Woolfrey, John,Sinha, Uma,Wong, Paul W.,Edwards, Susan T.,Arfsten, Ann E.,Clizbe, Lane A.,Kanter, James,Pandey, Anjali,Park, Gary,Hutchaleelaha, Athiwat,Lambing, Joseph L.,Hollenbach, Stanley J.,Scarborough, Robert M.,Zhu, Bing-Yan
scheme or table, p. 2179 - 2185 (2009/12/07)
Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were performed by modifying each of the three phenyl rings. A class of highly potent, selective, efficacious and orally bioavailable direct factor Xa inhibitors was discovered. These compounds were screened in hERG binding assays to examine the effects of substitution groups on the hERG channel affinity. From the leading compounds, betrixaban (compound 11, PRT054021) has been selected as the clinical candidate for development.
AROMATIC AMIDES
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, (2008/06/13)
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
